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Screening, Characterization and Evaluation of Mangiferin Polymorphs.
Shiying Yang1, Qi Zhou1, Baoxi Zhang1
1Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
This study identified five solid forms of mangiferin, including three new ones. Form V is recommended as the primary polymorph for developing new mangiferin-based pharmaceuticals due to its stability and solubility.
Area of Science:
- Pharmacology and Pharmaceutical Sciences
- Solid-State Chemistry
- Materials Science
Background:
- Mangiferin, a compound with diverse pharmacological activities, is found in numerous natural products.
- Previous literature reported anhydrous and hydrate forms of mangiferin separately, but its polymorphism was not fully understood.
- Polymorphism is crucial for drug development, affecting stability, solubility, and bioavailability.
Purpose of the Study:
- To conduct a comprehensive polymorph screening of mangiferin.
- To identify, characterize, and compare different solid-state forms of mangiferin.
- To evaluate the stability, transformation, and solubility of mangiferin polymorphs for pharmaceutical applications.
Main Methods:
- Polymorph screening using various solid-state characterization techniques.
- Powder X-ray diffraction (PXRD) for structural identification.
- Differential scanning calorimetry (DSC) and thermogravimetry (TGA) for thermal analysis.
- Hirshfeld surface analysis for intermolecular interactions.
Main Results:
- Five distinct solid forms of mangiferin were obtained, with three being novel discoveries.
- Characterization confirmed the identity and properties of each form.
- Crystallographic data and Hirshfeld surface analysis were reported for anhydrous and hydrate forms.
- Form V demonstrated favorable stability, transformation, and solubility profiles.
Conclusions:
- The study revealed the complex polymorphism of mangiferin.
- Form V emerged as a promising candidate for pharmaceutical development due to its advantageous properties.
- This research provides a foundation for the rational design of mangiferin-based drug products.
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